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Results for "

brain-penetrating

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (3) Aminopeptidase (2) Amyloid-β (1) Aryl Hydrocarbon Receptor (1) Calcium Channel (1) CaMK (1) Cholinesterase (ChE) (1) Deubiquitinase (1) Dopamine Receptor (2) Endogenous Metabolite (1) HDAC (1) Histamine Receptor (5) Insulin Receptor (1) LDLR (1) LRRK2 (1) mGluR (1) Mitophagy (1) Neurokinin Receptor (1) Opioid Receptor (2) Orexin Receptor (OX Receptor) (1) Oxytocin Receptor (2) Peptide-Drug Conjugates (PDCs) (1) Phosphodiesterase (PDE) (2) Prokineticin Receptor (1) RIP kinase (1) TRP Channel (1)
By Research Areas:	Cancer (4) Cardiovascular Disease (4) Endocrinology (4) Inflammation/Immunology (3) Metabolic Disease (2) Neurological Disease (21)

By Targets:

5-HT Receptor (3)

Aminopeptidase (2)

Amyloid-β (1)

Aryl Hydrocarbon Receptor (1)

Calcium Channel (1)

CaMK (1)

Cholinesterase (ChE) (1)

Deubiquitinase (1)

Dopamine Receptor (2)

Endogenous Metabolite (1)

HDAC (1)

Histamine Receptor (5)

Insulin Receptor (1)

LDLR (1)

LRRK2 (1)

mGluR (1)

Mitophagy (1)

Neurokinin Receptor (1)

Opioid Receptor (2)

Orexin Receptor (OX Receptor) (1)

Oxytocin Receptor (2)

Peptide-Drug Conjugates (PDCs) (1)

Phosphodiesterase (PDE) (2)

Prokineticin Receptor (1)

RIP kinase (1)

TRP Channel (1)

By Research Areas:

Cancer (4)

Cardiovascular Disease (4)

Endocrinology (4)

Inflammation/Immunology (3)

Metabolic Disease (2)

Neurological Disease (21)

Inhibitors & Agonists

Peptides

Inhibitory Antibodies

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-111409

RIP1 kinase inhibitor 1	RIP kinase	Inflammation/Immunology
RIP1 kinase inhibitor 1 (compound 22) is a highly potent, orally available, and brain-penetrating RIP1 kinase inhibitor (pK_i=9.04) .

HY-14880B

Bavisant dihydrochloride hydrate JNJ31001074AAC; JNJ31001074 dihydrochloride hydrate	Histamine Receptor	Neurological Disease Endocrinology
Bavisant dihydrochloride hydrate (JNJ31001074AAC) is an orally active, potent, brain-penetrating and highly selective antagonist of the histamine H₃ receptor. Bavisant dihydrochloride hydrate can be used for attention-deficit hyperactivity disorder (ADHD) research .

HY-14880

Bavisant JNJ-31001074	Histamine Receptor	Neurological Disease Endocrinology
Bavisant (JNJ-31001074) is an orally active, potent, brain-penetrating and highly selective antagonist of the histamine H₃ receptor. Bavisant can be used for attention-deficit hyperactivity disorder (ADHD) research .

HY-111791

ACY-1083 1 Publications Verification	HDAC	Cancer
ACY-1083 is a selective and brain-penetrating HDAC6 inhibitor with an IC₅₀ of 3 nM and is 260-fold more selective for HDAC6 than all other classes of HDAC isoforms. ACY-1083 effectively reverses chemotherapy-induced peripheral neuropathy .

HY-N12038

Coumarinic acid	Amyloid-β Cholinesterase (ChE)	Neurological Disease
Coumarinic acid is a brain-penetrating inhibitor of AChE and β-amyloid. Coumarinic acid can be used in study anti-Alzheimer drug .

HY-151797

Ph-HTBA	CaMK	Neurological Disease
Ph-HTBA is a high-affinity, brain-penetrating modulator for CaMKIIα. Ph-HTBA has binding affinity for CaMKIIα with a K_d value of 757 nM. Ph-HTBA can be used for the research of ischemia and neurodegenerative disorders .

HY-120710

DNS-8254	Phosphodiesterase (PDE)	Neurological Disease
DNS-8254 is an oral active and brain-penetrating PDE2a inhibitor with the IC₅₀ of 8 nM. DNS-8254 shows memory enhancing effects in a rat model .

HY-105235A

Enadoline hydrochloride CI-977 hydrochloride	Opioid Receptor	Neurological Disease
Enadoline (CI-977) hydrochloride is a highly selective, brain-penetrating, and nonpeptide kappa-opioid receptor (KOR) agonist (K_i=1.25 nM). Antinociceptive effects .

HY-105235

Enadoline CI-977	Opioid Receptor	Neurological Disease
Enadoline (CI-977) is a highly selective, brain-penetrating, and nonpeptide kappa-opioid receptor (KOR) agonist (K_i=1.25 nM). Antinociceptive effects .

HY-14880A

Bavisant dihydrochloride JNJ-31001074 dihydrochloride	Histamine Receptor	Neurological Disease Endocrinology
Bavisant (JNJ-31001074) dihydrochloride is an orally active, potent, brain-penetrating and highly selective antagonist of the histamine H₃ receptor. Bavisant dihydrochloride can be used for attention-deficit hyperactivity disorder (ADHD) research .

HY-137440B

(2R,3R)-Firazorexton (2R,3R)-TAK-994 free base	Orexin Receptor (OX Receptor)	Neurological Disease
(2R,3R)-Firazorexton ((2R,3R)-TAK-994 free base) is an isomer of Firazorexton (HY-137440). Firazorexton is an orally active, brain-penetrating orexin type 2 receptor (OX2R) agonist that may improve narcolepsy-like symptoms ..

HY-19917

JNJ-39220675	Histamine Receptor	Neurological Disease
JNJ-39220675 is a selective and brain-penetrating histamine H3 receptor antagonist with activity in regulating alcohol stimulation and reward. JNJ-39220675 is effective in reducing alcohol intake and preference in alcohol-preferring rats. JNJ-39220675 does not affect the ataxic effects of alcohol, the rate of alcohol elimination, or alcohol-induced nucleocapsid dopamine release .

HY-160019

MTX115325	Deubiquitinase Mitophagy	Neurological Disease
MTX115325 (Example 1) is an orally active, brain-penetrating USP30 inhibitor (IC₅₀=12 nM) with neuroprotective activity. MTX115325 increases ubiquitination (EC₅₀=32 nM) of the mitochondrial outer membrane protein TOM20 (a USP30 substrate), increasing mitophagy. MTX115325 prevents dopaminergic neuron loss and preserves striatal dopamine .

HY-P4073

ANG1005 GRN1005; Paclitaxel trevatide	Peptide-Drug Conjugates (PDCs) LDLR	Cancer
ANG1005 (Paclitaxel trevatide) is a brain-penetrating peptide-drug conjugate. ANG1005, a taxane derivative, consists of three paclitaxel (HY-B0015) molecules covalently linked to Angiopep-2, designed to cross the blood-brain and blood-cerebrospinal barriers and to penetrate malignant cells via low density lipoprotein receptor-related protein (LRP1) transport system .

HY-109118A

Masupirdine mesylate SUVN-502 mesylate	5-HT Receptor	Neurological Disease
Masupirdine mesylate (SUVN-502 mesylate) is a potent, selective, orally active, and brain-penetrating 5-HT₆ receptor antagonist (K_i of 2.04 nM for human 5-HT₆ receptor). Masupirdine mesylate has pro-cognitive effects on all stages of cognition (acquisition, consolidation, and retention), and can reverse Scopolamine (HY-N0296), MK-801 (HY-15084B)-induced and aging-related memory deficits. Masupirdine mesylate can be used in the research of Alzheimer's disease .

HY-109118

Masupirdine free base SUVN-502 free base	5-HT Receptor	Neurological Disease
Masupirdine free base (SUVN-502 free base) is a potent, selective, orally active, and brain-penetrating 5-HT₆ receptor antagonist (K_i of 2.04 nM for human 5-HT₆ receptor). Masupirdine free base has pro-cognitive effects on all stages of cognition (acquisition, consolidation, and retention), and can reverse Scopolamine (HY-N0296), MK-801 (HY-15084B)-induced and aging-related memory deficits. Masupirdine free base can be used in the research of Alzheimer's disease .

HY-125087

A-304121	Histamine Receptor	Neurological Disease
A-304121 is a selective and brain penetrating H3 receptor antagonist. A-304121 is a cognition-enhancing agent .

HY-153964

PF-06478939	Oxytocin Receptor	Cardiovascular Disease
PF-06478939 is a non-brain-penetrating peptide that is an agonist at oxytocin (OT) receptor and vasopressin receptor with EC₅₀ values of 0.01 nM and 0.078 nM, respectively .

HY-153964A

PF-06478939 TFA	Oxytocin Receptor	Cardiovascular Disease
PF-06478939 TFA is a non-brain-penetrating peptide that is an agonist at oxytocin (OT) receptor and vasopressin receptor with EC₅₀ values of 0.01 nM and 0.078 nM, respectively .

HY-112723

Apinocaltamide ACT-709478	Calcium Channel	Neurological Disease
Apinocaltamide (ACT-709478) is a potent, selective, orally active, and brain penetrating T-type calcium channel blocker. ACT-709478 is used in the research of generalized epilepsies .

HY-161571

LRRK2-IN-13	LRRK2	Neurological Disease
LRRK2-IN-13 (Compound 13) is an inhibitor of LRRK2 (IC₅₀=0.57 nM). LRRK2-IN-13 has brain penetrating properties .

HY-P99530

Valanafusp alfa AGT-181; HIRMAb-IDUA	Insulin Receptor	Metabolic Disease
Valanafusp alfa (AGT-181) is a chimeric monoclonal antibody that fuses human α-L-iduronidase (IDUA) and targets the human insulin receptor (HIR). Valanafusp alfa has brain penetrating properties, making it useful for research on mucopolysaccharidosis type I (MPS I) .

HY-109058

Firibastat 1 Publications Verification QGC001; RB150	Aminopeptidase	Cardiovascular Disease
Firibastat (QGC001), an orally active brain penetrating proagent of EC33, is a first-in-class brain aminopeptidase A (APA) inhibitor (K_i=200 nM). Firibastat selectively and specifically inhibits conversion of brain angiotensin-II into angiotensin-III and decreases blood pressure in hypertensive rats .

HY-148236

BAY-390 1 Publications Verification	TRP Channel	Inflammation/Immunology
BAY-390, a chemical probe, is a selective, across species active and brain penetrating TRPA1 inhibitor. BAY-390 inhibits hTRPA1 FLIPR, hTRPA1 Ephys, rTRPA1 FLIPR and rDRG Ephys with IC₅₀s of 16, 82, 63 and 35 nM, respectively. BAY-390 can be used for the research of inflammation .

HY-128349

MT-3014	Phosphodiesterase (PDE)	Neurological Disease
MT-3014 is a potent, highly selective and brain-penetrated phosphodiesterase 10A (PDE 10A) inhibitor, with IC₅₀s of 0.062 nM and 0.09 nM for human PDE 10A and bovine PDE 10A, respectively .

HY-147056B

PKRA83 hydrochloride PKRA7 hydrochloride	Prokineticin Receptor	Inflammation/Immunology Cancer
PKRA83 (PKRA7) hydrochloride is a potent, blood-brain-penetrating PK2 antagonist that competes for PK2 binding to its receptors, PKR1 and PKR2. PKRA83 hydrochloride potently inhibits PK2 receptors with IC₅₀ values of 5.0 nM and 8.2 nM for PKR1 and PKR2, respectively. PKRA83 hydrochloride exhibits anticancer, antiarthritis, and antiangiogenic activities .

HY-109058R

Firibastat (Standard)	Aminopeptidase	Cardiovascular Disease
Firibastat (Standard) is the analytical standard of Firibastat. This product is intended for research and analytical applications. Firibastat (QGC001), an orally active brain penetrating proagent of EC33, is a first-in-class brain aminopeptidase A (APA) inhibitor (Ki=200 nM). Firibastat selectively and specifically inhibits conversion of brain angiotensin-II into angiotensin-III and decreases blood pressure in hypertensive rats .

HY-100605

VU0483605	mGluR	Others
VU0483605 is a potent and brain-penetrated mGlu₁ receptor positive allosteric modulator (PAM). VU0483605 shows excellent mGlu₁ PAM activity at both human and rat, with EC₅₀ values of 390 and 356 nM, respectively .

HY-12697

NGB 2904	Dopamine Receptor	Neurological Disease
NGB 2904 is a potent, selective, orally active and brain-penetrated antagonist of dopamine D3 receptor, with a K_i of 1.4 nM. NGB 2904 shows selectivity for D3 over D2, 5-HT2, α1, D4, D1 and D5 receptors (K_is=217, 223, 642, >5000, >10000 and >10000 nM, respectively). NGB 2904 antagonizes Quinpirole-stimulated mitogenesis .

HY-12697A

NGB 2904 hydrochloride	Dopamine Receptor	Neurological Disease
NGB 2904 hydrochloride is a potent, selective, orally active and brain-penetrated antagonist of dopamine D3 receptor, with a K_i of 1.4 nM. NGB 2904 hydrochloride shows selectivity for D3 over D2, 5-HT2, α1, D4, D1 and D5 receptors (K_is=217, 223, 642, >5000, >10000 and >10000 nM, respectively). NGB 2904 hydrochloride antagonizes Quinpirole-stimulated mitogenesis .

HY-107691

GR 159897	Neurokinin Receptor	Neurological Disease Endocrinology Cancer
GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK₂) receptor antagonist. GR 159897 has little or no affinity for NK₁ and NK₃ receptors. GR 159897 inhibits binding of [ ³H]GR100679 to human NK₂ (hNK₂)-CHO cells and rat colon membranes with pK_is of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects .

HY-B2132

Tryptamine 1 Publications Verification 3-(2-Aminoethyl)indole~2-(3-Indolyl)ethylamine	Endogenous Metabolite 5-HT Receptor Aryl Hydrocarbon Receptor	Neurological Disease Metabolic Disease
Tryptamine is a selective, blood-brain-penetrating 5-HT4 receptor agonist (EC50=1-3 mM) and an endogenous ligand of the aryl hydrocarbon receptor (AHR) (Kd=10-50 nM). Tryptamine promotes intestinal anion secretion and fluid transport by activating G protein-coupled receptors (GPCRs) and accelerates gastrointestinal motility. Tryptamine regulates Th17/Treg balance to inhibit neuroinflammation, competitively binds to 5-HT receptors to regulate central nervous system activity, and participates in temperature regulation and spinal reflex regulation as a neuromodulator. Tryptamine can be used to study intestinal motility disorders such as functional constipation, and has shown significant efficacy in multiple sclerosis models .

Cat. No.	Product Name	Target	Research Area

HY-P4073

ANG1005 GRN1005; Paclitaxel trevatide	Peptide-Drug Conjugates (PDCs) LDLR	Cancer
ANG1005 (Paclitaxel trevatide) is a brain-penetrating peptide-drug conjugate. ANG1005, a taxane derivative, consists of three paclitaxel (HY-B0015) molecules covalently linked to Angiopep-2, designed to cross the blood-brain and blood-cerebrospinal barriers and to penetrate malignant cells via low density lipoprotein receptor-related protein (LRP1) transport system .

Cat. No.	Product Name	Target	Research Area

HY-P99530

Valanafusp alfa AGT-181; HIRMAb-IDUA	Insulin Receptor	Metabolic Disease
Valanafusp alfa (AGT-181) is a chimeric monoclonal antibody that fuses human α-L-iduronidase (IDUA) and targets the human insulin receptor (HIR). Valanafusp alfa has brain penetrating properties, making it useful for research on mucopolysaccharidosis type I (MPS I) .

Tryptamine 1 Publications Verification 3-(2-Aminoethyl)indole~2-(3-Indolyl)ethylamine	Alkaloids Microorganisms Classification of Application Fields Other Diseases Endogenous metabolite Disease Research Fields Indole Alkaloids	Endogenous Metabolite 5-HT Receptor Aryl Hydrocarbon Receptor
Tryptamine is a selective, blood-brain-penetrating 5-HT4 receptor agonist (EC50=1-3 mM) and an endogenous ligand of the aryl hydrocarbon receptor (AHR) (Kd=10-50 nM). Tryptamine promotes intestinal anion secretion and fluid transport by activating G protein-coupled receptors (GPCRs) and accelerates gastrointestinal motility. Tryptamine regulates Th17/Treg balance to inhibit neuroinflammation, competitively binds to 5-HT receptors to regulate central nervous system activity, and participates in temperature regulation and spinal reflex regulation as a neuromodulator. Tryptamine can be used to study intestinal motility disorders such as functional constipation, and has shown significant efficacy in multiple sclerosis models .

Coumarinic acid	Monophenols Microorganisms Ketones, Aldehydes, Acids Source classification Phenols	Amyloid-β Cholinesterase (ChE)
Coumarinic acid is a brain-penetrating inhibitor of AChE and β-amyloid. Coumarinic acid can be used in study anti-Alzheimer drug .

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